Caspofungin

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  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 162808-62-0
  • AHFC code: 08:14.2
  • Synonyms: (4R,5S)-5-((2-Aminoethyl)amino)-N(sup 2)-(10,12-dimethyltetradecanoyl)-4-hydroxy-L-ornithyl-L-threonyl-trans-4-hydroxy-L-prolyl-(S)-4-hydroxy-4-(p-hydroxyphenyl)-L-threonyl-threo-3-hydroxy-L-ornithyl-trans-3-hydroxy-L-proline cyclic (6-1)-peptide, Cancidas, Caspofungin, HSDB 7476, L 743,872, L 743872, MK 0991, UNII-F0XDI6ZL63
  • ATC Code: J02AX04
  • Chemical Formula: C52-H88-N10-O15
  • Molecular Weight: 1093.32
  • Assay/Purity: Typically NLT 98%
  • DrugBank: APRD00199
  • SMILES: C(CN)[C,H]([C,,H]1NC(=O)[C,,H]([C,H](O)[C,H](c2ccc(cc2)O)O)NC([C,H]2N(C([C,,H]([C,H](O)C)NC(=O)[C,,H](NC(=O)CCCCCCCC[C,,H](C)C[C,,H](C)CC)C[C,H]([C,,H](NC([C,,H]3[C,H](CCN3C1=O)O)=O)NCCN)O)=O)C[C,,H](C2)O)=O)O
  • InChl:
  • PubChem: 468682
  • IUPAC:

Additional Details

Indication:
For the treatment of esophageal candidiasis and invasive aspergillosis in patients who are refractory to or intolerant of other therapies.
Pharmacodynamics:
Caspofungin is an antifungal drug, and belongs to a new class termed the echinocandins. It is used to treat Aspergillus and Candida infection, and works by inhibiting cell wall synthesis. Antifungals in the echinocandin class inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3-beta glucan synthase. There is a potential for resistance development to occur, however in vitro resistance development to Caspofungin by Aspergillus species has not been studied.
Mode of Action:
Caspofungin inhibits the synthesis of beta-(1,3)-D-glucan, an essential component of the cell wall of Aspergillus species and Candida species. beta-(1,3)-D-glucan is not present in mammalian cells. The primary target is beta-(1,3)-glucan synthase.
Metabolism:
Metabolized slowly by hydrolysis and N-acetylation
Toxicity:
Side effects include rash, swelling, and nausea (rare)
General Reference:
Letscher-Bru, Valérie, and Raoul Herbrecht. 2003. Caspofungin: the first representative of a new antifungal class. Journal of Antimicrobial Chemotherapy 51, no. 3 (March 1): 513 -521. doi:10.1093/jac/dkg117.Sucher AJ, Chahine EB, Balcer HE: Echinocandins: the newest class of antifungals. Ann Pharmacother. 2009 Oct;43(10):1647-57. Epub 2009 Sep 1. PubmedMorrison VA: Caspofungin: an overview. Expert Rev Anti Infect Ther. 2005 Oct;3(5):697-705. PubmedMcCormack PL, Perry CM: Caspofungin: a review of its use in the treatment of fungal infections. Drugs. 2005;65(14):2049-68. PubmedMorris MI, Villmann M: Echinocandins in the management of invasive fungal infections, part 1. Am J Health Syst Pharm. 2006 Sep 15;63(18):1693-703. PubmedMorris MI, Villmann M: Echinocandins in the management of invasive fungal infections, Part 2. Am J Health Syst Pharm. 2006 Oct 1;63(19):1813-20. Pubmed
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